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Chemical Compound Review

Diaberit     3-(diaminomethylidene)-1,1- dimethyl...

Synonyms: Diabesin, Diabetex, Diaphage, Diformin, Fortamet, ...
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Disease relevance of metformin

 

High impact information on metformin

 

Chemical compound and disease context of metformin

 

Biological context of metformin

 

Anatomical context of metformin

  • Oral absorption of the antihyperglycaemic agent metformin hydrochloride (MF-HCl) is confined to the upper part of the intestine, therefore rational controlled-release formulations of this drug should ensure a complete release during transit from stomach to jejunum [15].
  • Restricted delivery of metformin hydrochloride to the small intestine from differently coated pellets resulted in increased relative bioavailability and a sustained release effect [16].
 

Associations of metformin with other chemical compounds

  • Beyond its antidiabetic activity justifying its use in the treatment of the type 2 diabetes, metformin (MET [dimethylguanidine, Glucophage]) has been shown to exhibit antioxidant properties in vitro, which could contribute to limit the deleterious vascular complications of diabetes [17].
  • The combination of glucophage and doanil tablets resulted in synergistic effect producing 59 +/- 9.27% reduction in plasma glucose levels by 4h and significantly higher (P < 0.001) AUC and RH compared to either of the tablets alone [14].
  • Moreover, the 90% confidence interval for the ratio of the logarithmic transformed AUC0-infinity values, as well as the logarithmic transformed Cmax values, of Diabetmin Retard over those of Glucophage Retard was within the acceptance criteria of 0.80-1.25 [18].
 

Gene context of metformin

 

Analytical, diagnostic and therapeutic context of metformin

References

  1. Lactic acidosis associated with Glucophage use in a man with normal renal and hepatic function. Pepper, G.M., Schwartz, M. Diabetes Care (1997) [Pubmed]
  2. Cholestatic jaundice associated with the use of metformin. Desilets, D.J., Shorr, A.F., Moran, K.A., Holtzmuller, K.C. Am. J. Gastroenterol. (2001) [Pubmed]
  3. Metformin hydrochloride in the treatment of type 2 diabetes mellitus: a clinical review with a focus on dual therapy. Setter, S.M., Iltz, J.L., Thams, J., Campbell, R.K. Clinical therapeutics. (2003) [Pubmed]
  4. What is the role of combination therapy (insulin plus oral medication) in type 2 diabetes? Eskesen, S., Kelsberg, G., Hitchcock, K., Lo, V. The Journal of family practice (2006) [Pubmed]
  5. Psoriasiform drug eruption associated with metformin hydrochloride: a case report. Koca, R., Altinyazar, H.C., Yenidünya, S., Tekin, N.S. Dermatol. Online J. (2003) [Pubmed]
  6. Rapid liquid-chromatographic determination of metformin in plasma and urine. Charles, B.G., Jacobsen, N.W., Ravenscroft, P.J. Clin. Chem. (1981) [Pubmed]
  7. Metformin (Glucophage) inhibits tyrosine phosphatase activity to stimulate the insulin receptor tyrosine kinase. Holland, W., Morrison, T., Chang, Y., Wiernsperger, N., Stith, B.J. Biochem. Pharmacol. (2004) [Pubmed]
  8. Pharmacokinetics of metformin gastric-retentive tablets in healthy volunteers. Gusler, G., Gorsline, J., Levy, G., Zhang, S.Z., Weston, I.E., Naret, D., Berner, B. Journal of clinical pharmacology. (2001) [Pubmed]
  9. Design and evaluation of compound metformin/glipizide elementary osmotic pump tablets. Ouyang, D., Nie, S., Li, W., Guo, H., Liu, H., Pan, W. J. Pharm. Pharmacol. (2005) [Pubmed]
  10. Plasminogen activator inhibitor activity, 4G5G polymorphism of the plasminogen activator inhibitor 1 gene, and first-trimester miscarriage in women with polycystic ovary syndrome. Glueck, C.J., Sieve, L., Zhu, B., Wang, P. Metab. Clin. Exp. (2006) [Pubmed]
  11. Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: bridging evidence for metformin immediate-release tablet. Cheng, C.L., Yu, L.X., Lee, H.L., Yang, C.Y., Lue, C.S., Chou, C.H. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. (2004) [Pubmed]
  12. Subchronic treatment with metformin produces anorectic effect and reduces hyperinsulinemia in genetically obese Zucker rats. Rouru, J., Huupponen, R., Pesonen, U., Koulu, M. Life Sci. (1992) [Pubmed]
  13. Metformin hydrochloride: an antihyperglycemic agent. Klepser, T.B., Kelly, M.W. American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists. (1997) [Pubmed]
  14. Enteric-coated insulin capsules: a combination with or a replacement of oral hypoglycaemic drugs. Hosny, E.A., el-Bagory, I.M., al-Jenoobi, F.I. Bollettino chimico farmaceutico. (2002) [Pubmed]
  15. A site-specific controlled-release system for metformin. Di Colo, G., Zambito, Y., Baggiani, A., Carelli, V., Serafini, M.F. J. Pharm. Pharmacol. (2005) [Pubmed]
  16. Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets. Hu, L.D., Liu, Y., Tang, X., Zhang, Q. European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V. (2006) [Pubmed]
  17. Metformin decreases intracellular production of reactive oxygen species in aortic endothelial cells. Ouslimani, N., Peynet, J., Bonnefont-Rousselot, D., Thérond, P., Legrand, A., Beaudeux, J.L. Metab. Clin. Exp. (2005) [Pubmed]
  18. Relating in vitro/in vivo data of two controlled-release metformin formulations. Yuen, K.H., Peh, K.K., Tan, B.L. Drug development and industrial pharmacy. (1999) [Pubmed]
  19. Bioequivalence of a generic metformin tablet preparation. Yuen, K.H., Wong, J.W., Billa, N., Julianto, T., Toh, W.T. International journal of clinical pharmacology and therapeutics. (1999) [Pubmed]
  20. Metformin hydrochloride and recurrent miscarriage in a woman with polycystic ovary syndrome. Palomba, S., Falbo, A., Orio, F., Russo, T., Tolino, A., Zullo, F. Fertil. Steril. (2006) [Pubmed]
  21. Use of cellulose ether containing excipients with microcrystalline cellulose for the production of pellets containing metformin hydrochloride by the process of extrusion-spheronization. Gouldson, M.P., Deasy, P.B. Journal of microencapsulation. (1997) [Pubmed]
  22. Metformin hydrochloride in patients undergoing myelography. Henry, W.D. AJR. American journal of roentgenology. (2002) [Pubmed]
 
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